基于优势吲哚骨架的α淀粉酶抑制剂的合成。
Synthesis of alpha amylase inhibitors based on privileged indole scaffold.
作者信息
Noreen Tayyaba, Taha Muhammad, Imran Syahrul, Chigurupati Sridevi, Rahim Fazal, Selvaraj Manikandan, Ismail Nor Hadiani, Mohammad Jahidul Islam, Ullah Hayat, Javid Muhammad Tariq, Nawaz Faisal, Irshad Maryam, Ali Muhammad
机构信息
Department of Chemistry, University of Wah, Quaid Avenue, Wah Cantt 47000, Pakistan; Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor, Malaysia.
Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor, Malaysia; Faculty of Applied Science, UiTM Shah Alam, 40450 Shah Alam, Selangor D.E., Malaysia.
出版信息
Bioorg Chem. 2017 Jun;72:248-255. doi: 10.1016/j.bioorg.2017.04.010. Epub 2017 Apr 21.
Twenty five derivatives of indole carbohydrazide (1-25) had been synthesized. These compounds were characterized using H NMR and EI-MS, and further evaluated for their α-amylase inhibitory potential. The analogs (1-25) showed varying degree of α-amylase inhibitory potential. ranging between 9.28 and 599.0µM when compared with standard acarbose having IC value 8.78±0.16µM. Six analogs, 25 (IC=9.28±0.153µM), 22 (IC=9.79±0.43µM), 4 (IC=11.08±0.357µM), 1 (IC=12.65±0.169µM), 8 (IC=21.37±0.07µM) and 14 (IC=43.21±0.14µM) showed potent α-amylase inhibition as compared to the standard acarbose (IC=8.78±0.16µM). All other analogs displayed good to moderate inhibitory potential. Structure-activity relationship was established through the interaction of the active compounds with enzyme active site with the help of docking studies.
已合成了25种吲哚碳酰肼衍生物（1 - 25）。这些化合物通过核磁共振氢谱（H NMR）和电子轰击质谱（EI - MS）进行了表征，并进一步评估了它们对α - 淀粉酶的抑制潜力。类似物（1 - 25）表现出不同程度的α - 淀粉酶抑制潜力。与具有8.78±0.16µM IC值的标准阿卡波糖相比，其抑制潜力在9.28至599.0µM之间。与标准阿卡波糖（IC = 8.78±0.16µM）相比，6种类似物，即25（IC = 9.28±0.153µM）、22（IC = 9.79±0.43µM）、4（IC = 11.08±0.357µM）、1（IC = 12.65±0.169µM）、8（IC = 21.37±0.07µM）和14（IC = 43.21±0.14µM）表现出较强的α - 淀粉酶抑制作用。所有其他类似物显示出良好至中等的抑制潜力。通过对接研究，借助活性化合物与酶活性位点的相互作用建立了构效关系。
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